Oral Pharmacokinetics of Bisoprolol in Resting and Exercising Healthy Volunteers
| Autor: | Patrice Jaillon, B. Lecocq, P Sauleman, A Rames, J L Cuche, Jean-Marie Poirier, F Le Coz, M Midavaine |
|---|---|
| Rok vydání: | 1991 |
| Předmět: |
Adult
Male Adrenergic beta-Antagonists Cmax Blood Pressure Physical exercise Pharmacology Propanolamines Norepinephrine Catecholamines Pharmacokinetics Heart Rate Oral administration medicine Bisoprolol Humans Dosing Exercise Volunteer business.industry Crossover study Anesthesia Exercise Test Cardiology and Cardiovascular Medicine business Half-Life medicine.drug |
| Zdroj: | Journal of Cardiovascular Pharmacology. 18:28-34 |
| ISSN: | 0160-2446 |
| DOI: | 10.1097/00005344-199107000-00005 |
| Popis: | The effects of exercise on bisoprolol oral pharmacokinetics were studied in eight healthy male volunteers in an open, randomized, three-period, crossover trial. Oral bisoprolol (20 mg) was given either at rest during 24 h or with iterative stress tests before and 2.5, 5, 10, and 24 h after dosing. Exercise tests were repeated on a third placebo period. Bisoprolol was assayed in plasma and urines, and plasma catecholamines were measured before and after stress tests, Cmax, Tmax, elimination t1/2, and renal clearance of bisoprolol were not significantly modified by exercise. AUC0-infinity significantly decreased by 7.5% (p less than 0.05) with stress test resulting in an increase in apparent oral clearance. The beta-blocking effect peaked at 2.5 h, lasted greater than 24 h, and was related to plasma levels. The exercise-induced increase in plasma norepinephrine levels was significantly augmented with bisoprolol. These results suggest that repeated exercise tests exerted only limited effects on the oral pharmacokinetics of bisoprolol. |
| Databáze: | OpenAIRE |
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